Gu Yuan, Zhao Zheng, Niu Guangle, Zhang Han, Wang Yiming, Kwok Ryan T K, Lam Jacky W Y, Tang Ben Zhong
Department of Chemical and Biological Engineering , Department of Chemistry , The Hong Kong Branch of Chinese National Engineering Research Center for Tissue Restoration and Reconstruction , Institute for Advanced Study , The Hong Kong University of Science and Technology , Clear Water Bay , Kowloon , Hong Kong 999077 , China . Email:
HKUST-Shenzhen Research Institute , No. 9 Yuexing 1st RD, South Area Hi-tech Park , Nanshan , Shenzhen 518057 , China.
Chem Sci. 2020 May 15;11(22):5753-5758. doi: 10.1039/d0sc02097d. eCollection 2020 Jun 14.
In clinical chemotherapy, some basic drugs cannot enter the hydrophobic cell membrane because of ionization in the acidic tumor microenvironment, a phenomenon known as ion trapping. In this study, we developed a method to visualize this ion trapping phenomenon by utilizing a pH-responsive ratiometric AIEgen, dihydro berberine (). By observing the intracellular fluorescence of , we found that non-ionized can enter cells more easily than ionized forms, which is in accordance with the concept of ion trapping. In addition, shows superior anti-photobleaching ability to thanks to its AIE properties. These results suggest that can serve as a bioprobe for ion trapping.
在临床化疗中,一些碱性药物由于在酸性肿瘤微环境中发生离子化而无法进入疏水细胞膜,这种现象称为离子捕获。在本研究中,我们开发了一种方法,通过利用pH响应型比率荧光团二氢黄连素()来可视化这种离子捕获现象。通过观察的细胞内荧光,我们发现非离子化的比离子化形式更容易进入细胞,这与离子捕获的概念一致。此外,由于其聚集诱导发光(AIE)特性,在抗光漂白能力方面优于。这些结果表明可作为离子捕获的生物探针。